Alkylating agents Flashcards
Busulfan
AD VERSEEFFECT S
Severe myelosuppression (in almost all cases), pulmonary
fibrosis, hyperpigmentation
Busulfan
MECHANISM
Cross-links DNA
Nitrogen mustards
Cyclophosphamide,
ifosfamide
MECHANISM
Cross-link DNA
Require bioactivation by liver
Nitrogen mustards
Cyclophosphamide,
ifosfamide
AD VERSEEFFECT S
Myelosuppression, SIADH, Fanconi syndrome
(ifosfamide), hemorrhagic cystitis and bladder cancer
(prevent with mesna)
Nitrosoureas
Carmustine, lomustine
MECHAN ISM
Cross-link DNA Require bioactivation by liver
Cross blood-brain barrier
Nitrosoureas
Carmustine, lomustine
AD VERSEEFFECT S
CNS toxicity (convulsions,
dizziness, ataxia)
Procarbazine
mechanism
Mechanism unknown
Weak MAO inhibitor
procarbazine
adverseffect
Myelosuppression, pulmonary
toxicity, leukemia, disulfiramlike reaction
Temozolomide
mechanism
DNA methylation
Temozolomide
adverseffect
Myelosuppression
Platinum compounds
Cisplatin, carboplatin, oxaliplatin.
MECHANISM
Cross-link DNA. Cell cycle nonspecific.
Platinum compounds
Cisplatin, carboplatin, oxaliplatin.
AD VERSE EFFECT S
Nephrotoxicity (eg, Fanconi syndrome; prevent with amifostine), peripheral neuropathy, ototoxicity.
Taxanes
Docetaxel, paclitaxel
mechanism
Hyperstabilize polymerized microtubules → prevent mitotic spindle breakdown
Taxanes
Docetaxel, paclitaxel
AD VERSEEFFECT S
Myelosuppression, neuropathy,
hypersensitivity
Vinca alkaloids
Vincristine, vinblastine
mechanism
Bind β-tubulin and inhibit
its polymerization into
microtubules → prevent
mitotic spindle formation
Vinca alkaloids
Vincristine, vinblastine
adverseffect
Vincristine (crisps the nerves):
neurotoxicity (axonal
neuropathy), constipation
(including ileus)
Vinblastine (blasts the
marrow): myelosuppression
Irinotecan, topotecan
mechanism
Inhibit topoisomerase I
Irinotecan, topotecan
adverseffect
Severe myelosuppression,
diarrhea
Etoposide, teniposide
mechanism
Inhibit topoisomerase II
Etoposide, teniposide
adverseffects
Myelosuppression, alopecia
Tamoxifen
mechanism
antagonist in breast tissue,
partial agonist in endometrium and bone
Tamoxifen
adverseffects
Hot flashes, increase risk of thromboembolic events (eg, DVT, PE) and endometrial cancer.
